Pharmacokinetics and pharmacodynamics of stereoisomeric drugs with particular reference to bioequivalence determination

Peter Lees (1) , Robert Hunter (2) , Phil Reeves (3) , Pierre-Louis Toutain (4)

1 Royal Veterinary College
2 Food Animal Therapeutics
3 Australian Pesticides & Veterinary Medicines Authority
4 ToxAlim - ToxAlim

Drugs containing one or more chiral centres exist in stereoisomeric molecular forms. Most commonly, drugs containing a single asymmetric carbon atom exist in two enantiomeric forms, designated as eutomer (the more potent) and distomer(the less potent). As well as differences in potency and other pharmacodynamic properties, most members of enantiomeric pairs commonly differ also in their pharmacokinetic profiles. This article reviews factors underlying differences in pharmacological properties of enantiomers. The relevance of such differences for studies designed to evaluate the bioequivalence of products containing chiral drugs is also reviewed.

Mots clés: STEREOCHEMISTRY; ALBENDAZOLE; CHIRAL INVERSION; IBUPROFEN ENANTIOMERS; COMPARATIVE BIOAVAILABILITY; RACEMIC DRUGS; NONSTEROIDAL ANTIINFLAMMATORY DRUGS; ENANTIOSELECTIVITY; ASSAYS; INDIVIDUAL BIOEQUIVALENCE

Domaines: Sciences du Vivant [q-bio]

Peter Lees, Robert Hunter, Phil Reeves, Pierre-Louis Toutain. Pharmacokinetics and pharmacodynamics of stereoisomeric drugs with particular reference to bioequivalence determination. Journal of Veterinary Pharmacology and Therapeutics, 2012, 35, pp.17-30. ⟨10.1111/j.1365-2885.2012.01367.x⟩. ⟨hal-01191249⟩